Luotonin A compound and preparation method and application thereof

A compound and reaction technology, applied in the field of Luotonin A series compounds and their preparation, can solve the problems of no clinical application value, low binding ability, low anti-tumor activity, etc., and achieve easy synthesis and preparation, stable structure, and strong anti-proliferation activity Effect
CN111454264AActive Publication Date: 2020-07-28HUBEI UNIV OF CHINESE MEDICINE
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
HUBEI UNIV OF CHINESE MEDICINE
Publication Date
2020-07-28

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Abstract

The invention relates to the technical field of medicinal chemistry, and discloses a Luotonin A compound and a preparation method and application thereof. The Luotonin A compound represented by formula (I) and a pharmaceutically acceptable salt thereof are disclosed. R1 is H or halogen, R2 is an ethylenediamine group, a C1-C6 alkyl substituted ethylenediamine group, a piperazinyl group, a C1-C6 alkyl substituted piperazinyl group, a morpholinyl group, a C1-C6 alkyl substituted morpholinyl group, a homopiperazinyl group or a C1-C6 alkyl substituted homopiperazinyl group, and X is C or N. The Luotonin A compound provided by the invention is stable in structure and easy to synthesize and prepare, can be used as a novel topoisomerase I inhibitor, and has relatively strong anti-proliferative activity on cell strains of liver cancer, lung cancer, breast cancer and cervical cancer.
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Description

technical field

[0001] The present invention relates to the technical field of medicinal chemistry, in particular to a Luotonin A series compound and its preparation method and application Background technique

[0002] Topoisomerase regulates important life processes of cells: transcription, translation, mitosis, and nucleic acid repair, etc., which widely exist in prokaryotes and eukaryotes. Humans encode six topoisomerases, which are divided into topoisomerase I (Topo I) and topoisomerase II (Topo II) according to their functions. Due to the frequent proliferation of tumor cells, Topo I is very active, while Topo I in normal cells is not active, making Topo I one of the important targets of antitumor drugs.

[0003] Camptothecin, extracted from the bark of Camptothecin, is the most representative topoisomerase I inhibitor. Today, most of its derivatives are clinically used, such as topotecan and irinotecan, for the treatment of colon cancer, ovarian cancer and small cell...

Claims

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